Keap1-IN-1

• Description:

  Keap1-IN-1 (Compound 27) is the inhibitor for Keap1, that covalently modifys the Cys151 site in the BTB domain of KEAP1, and interfers with the interaction between Keap-Nrf. Keap1-IN-1 upregulates the mRNA expression of the antioxidant stress element (ARE) -dependent gene NQO1 with an EC50 of 160 nM. Keap1-IN-1 exhibits cytotoxicity in cell U2OS with an EC50 of 527 nM[1].

• UNSPSC:

  12352005

• Target:

  Keap1-Nrf2; Quinone Reductase

• Related Pathways:

  Metabolic Enzyme/Protease; NF-κB

• Applications:

  Metabolism-protein/nucleotide metabolism

• Field of Research:

  Others

• Smiles:

  CCP1(CCN(C2=C(S(=O)(C3=C(Cl)C(Cl)=CC=C3)=O)N=C(S(=O)(CC)=O)S2)CC1)=O

• Molecular Formula:

  C17H21Cl2N2O5PS3

• Molecular Weight:

  531.43

• References & Citations:

  [1]Fejes I, et al., Covalent Inhibitors of KEAP1 with Exquisite Selectivity. J Med Chem. 2024 Dec 12;67 (23) :21208-21222.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported